生物活性 靶点 体外研究 体内研究 诺普利兰 试剂级价格
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诺普利兰

诺普利兰,61413-54-5,结构式
诺普利兰
  • CAS号:61413-54-5
  • 英文名:ROLIPRAM
  • 中文名:诺普利兰
  • CBNumber:CB2703866
  • 分子式:C16H21NO3
  • 分子量:275.34
  • MOL File:61413-54-5.mol
诺普利兰化学性质
  • 熔点 :127-133 °C
  • 沸点 :418.29°C (rough estimate)
  • 密度 :1.0677 (rough estimate)
  • 折射率 :1.5500 (estimate)
  • 储存条件 :Sealed in dry,Store in freezer, under -20°C
  • 溶解度 :H2O: 0.2 mg/mL
  • 形态 :solid
  • 酸度系数(pKa) :16.02±0.40(Predicted)
  • 颜色 :white to off-white
  • Merck :14,8251
  • 稳定性 :Stable for 2 years from date of purchase as supplied. Solutions in DMSO or ethanol may be stored at -20°C for up to 3 months.
安全信息
  • 危险品标志 :Xi
  • 危险类别码 :36/37/38-11
  • 安全说明 :26-36
  • 危险品运输编号 :3249
  • WGK Germany :3
  • RTECS号 :UY5749237
  • 危险等级 :6.1(b)
  • 包装类别 :III
  • 海关编码 :29337900
  • 毒性 :LD50 oral in mouse: > 300mg/kg

诺普利兰性质、用途与生产工艺

  • 生物活性 PDE4的选择性抑制剂,Rolipram (ZK-62711, SB 95952),抑制免疫纯化的PDE4B和PDE4D活性,IC50分别为130 nM和240 nM。具有抗炎活性。
  • 靶点
    TargetValue
    PDE4B
    (Cell-free assay)
    130 nM
    PDE4D
    (Cell-free assay)
    240 nM
  • 体外研究

    The PDE4 selective inhibitor, Rolipram, inhibits immunopurified PDE4B and PDE4D activities similarly, with IC 50 s of approx. 130 nM and 240 nM respectively. In contrast, Rolipram inhibits immunopurified PDE4A activity with a dramatically lower IC 50 of around 3 nM. Rolipram increases phosphorylation of cAMP-response-element-binding protein (CREB) in U937 cells in a dose-dependent fashion, which implies the presence of both high affinity (IC 50 approx. 1 nM) and low affinity (IC 50 approx. 120 nM) components. Rolipram dose-dependently inhibits the IFN-gamma-stimulated phosphorylation of p38 MAPK in a simple monotonic fashion with an IC 50 of approx. 290 nM. Rolipram is a selective PDE4 inhibitor that inhibits all PDE4 isoforms A, B, C and D. Rolipram inhibits LPS-induced TNF production in a dose-dependent manner (IC 50 25.9 nM), and maximal/submaximal inhibition is observed with 2 μM drug concentration in J774 cells.

  • 体内研究

    TNF mRNA and protein expression is induced by LPS in peritoneal macrophages (PM) from WT mice, and that is clearly (by 74 and 63% for TNF mRNA and TNF protein, respectively) inhibited by Rolipram. LPS-induced TNF production is enhanced in PM from MKP-1(-/-) mice as compared to that in PM from WT mice, which is in line with the published results. Interestingly, the inhibition of TNF mRNA and protein expression by Rolipram is markedly attenuated in PM from MKP-1(-/-) mice and does not reach statistical significance. Repeated administration of Rolipram (1.25 mg/kg, i.p.) reduces the number of escape failures in learned helplessness rats.

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诺普利兰 试剂级价格
  • 更新日期:2024/11/11
  • 产品编号:XW6141354502
  • 产品名称:咯利普兰
  • CAS编号:61413-54-5
  • 包装:500MG
  • 价格:1848元
  • 更新日期:2024/11/11
  • 产品编号:XW6141354501
  • 产品名称:咯利普兰
  • CAS编号:61413-54-5
  • 包装:100MG
  • 价格:636元
诺普利兰生产厂家
  • 公司名称:北京百灵威科技有限公司
  • 联系电话:010-82848833 400-666-7788
  • 电子邮件:jkinfo@jkchemical.com
  • 国家:中国
  • 产品数:94657
  • 优势度:76
  • 公司名称:凯试(上海)科技有限公司
  • 联系电话:021-50135380
  • 电子邮件:shchemsky@sina.com
  • 国家:中国
  • 产品数:15402
  • 优势度:60
  • 公司名称:Syntechem Co.,Ltd
  • 联系电话:
  • 电子邮件:info@syntechem.com
  • 国家:中国
  • 产品数:12984
  • 优势度:57
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